Ro 41-5253 是一种具有口服活性的选择性维甲酸受体RARα拮抗剂。Ro 41-5253 可以与 RARα 结合而不诱导转录或影响 RAR/RXR 异二聚化和 DNA 结合。Ro 415253 可抑制癌细胞增殖并诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。
| 生物活性 | Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affectingRAR/RXRheterodimerization and DNA binding. Ro 41-5253 can inhibitcancercell proliferation and induceapoptosis, has antitumor activity[1][2]. |
| IC50& Target | IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ)[3]. |
体外研究
(In Vitro) | Ro 41-5253 (1 nM-10 μM, 10 days) significantly inhibits MCF-7 and ZR 75.1 cell proliferation and induces cell apoptosis in a time and dose-dependent manner[1].
Cell Proliferation Assay[1] | Cell Line: | Human breast-carcinoma lines MCF-7 and ZR 75.1 | | Concentration: | 1 nM-10 μM | | Incubation Time: | 10 days | | Result: | Inhibited 81% MCF-7 cell growth at 10 μM, 30% cell growth at 1 μM and no significant inhibitory effect at concentrations below 0.1 μM.
Inhibited 74% ZR 75.1 cell growth at 10 μM, 63% cell growth at 1 μM and 42% cell growth at 0.1 μM. |
Apoptosis Analysis[1] | Cell Line: | Human breast-carcinoma lines MCF-7 and ZR 75.1 | | Concentration: | 1 nM-10 μM | | Incubation Time: | 10 days | | Result: | Induced 28.5, 21.6, 16 and 12% of MCF-7 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the fourth day while induced 58, 51, 36 and 21% of cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively after six days.
Induced 80, 65, 43 and 29% of ZR 75.1 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the sixth day. |
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体内研究
(In Vivo) | Ro 41-5253 (oral gavage, 10-600 mg/kg, once a week, 4 weeks) can reduce tumor volume in female athymic Balb/mice transplanted with MCF-7 cell line[2].
| Animal Model: | Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line[2] | | Dosage: | 10, 30, 100, 300 and 600 mg/kg | | Administration: | Oral gavage; once a week; 4 weeks | | Result: | Resulted in a reduction in tumor volume at doses of 10, 30 and 100 mg/kg with no toxic side effects. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(206.33 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0633 mL | 10.3167 mL | 20.6334 mL | | 5 mM | 0.4127 mL | 2.0633 mL | 4.1267 mL | | 10 mM | 0.2063 mL | 1.0317 mL | 2.0633 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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